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FORMULATION OF SUSTAINED RELEASE ZIDOVUDINE MATRIX TABLETS THROUGH OPTIMIZATION AND THEIR EVALUATION

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ABSTRACT

                The object of the present study was to prepare and evaluate sustained release zidovudine matrix tablets. Zidovudine, the first anti-HIV compound approved for clinical use is widely used for the treatment of AIDS either alone or in combination with other antiviral agents. However, the main limitation to therapeutic effectiveness of zidovudine is its dose-dependent hematological toxicity, low therapeutic index, short biological half-life, and poor bioavailability. Sustained release matrix tablets were prepared using combination of hydrophilic polymer HPMC K15M and hydrophobic polymer ethyl cellulose. Optimization techniques using factorial design for two factors at three levels (32 ) was selected to optimize varied response variables viz. release rate exponent (n),  k, amount of drug released in 12h (Rel12h) and mean dissolution time MDT.  The optimum formulation was selected and the results obtained with the experimental values were compared with the predicted values. In conclusion, the results suggest that the developed sustained-release matrix tablets could provide quite regulated release of zidovudine over an extended period of time12 hrs leading to improve efficacy and better patient compliance.

 

Key words: Zidovudine, Matrix tablets, HPMC, Sustained release.

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